EA200702626A1 - NEW SUBSTITUTE TETRACYCLIC DERIVATIVES OF TETRAHYDROFURANE, PYRROLIDINE AND TETRAHYDROTHIOPHENE AND THEIR APPLICATION AS A MEDICINE - Google Patents

NEW SUBSTITUTE TETRACYCLIC DERIVATIVES OF TETRAHYDROFURANE, PYRROLIDINE AND TETRAHYDROTHIOPHENE AND THEIR APPLICATION AS A MEDICINE

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Publication number
EA200702626A1
EA200702626A1 EA200702626A EA200702626A EA200702626A1 EA 200702626 A1 EA200702626 A1 EA 200702626A1 EA 200702626 A EA200702626 A EA 200702626A EA 200702626 A EA200702626 A EA 200702626A EA 200702626 A1 EA200702626 A1 EA 200702626A1
Authority
EA
Eurasian Patent Office
Prior art keywords
receptors
tetrahydrothiophene
pyrrolidine
medicine
tetrahydrofurane
Prior art date
Application number
EA200702626A
Other languages
Russian (ru)
Inventor
Антониус Адрианус Хендрикус Петрус Мегенс
Андрес Авелино Трабанко-Суарес
Мохамед Коукни
Джорж Жозеф Корнелиус Хорнарт
Франс Йозеф Корнелиус Компернолле
Томаш Козлецки
Хосе Мария Сид-Нуньес
Хуа Мао
Сушил Чандра Джха
Франсиско Хавьер Фернандес-Гадеа
Original Assignee
Янссен Фармацевтика Н.В.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Янссен Фармацевтика Н.В. filed Critical Янссен Фармацевтика Н.В.
Publication of EA200702626A1 publication Critical patent/EA200702626A1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C07D209/80—[b, c]- or [b, d]-condensed
    • C07D209/94—[b, c]- or [b, d]-condensed containing carbocyclic rings other than six-membered
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035—Isoindoles, e.g. phthalimide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/56—Ring systems containing three or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/93—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems condensed with a ring other than six-membered
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/94—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/78—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with rings other than six-membered or with ring systems containing such rings
    • C07D333/80—Seven-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Reproductive Health (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Anesthesiology (AREA)
  • Hematology (AREA)
  • Addiction (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyrane Compounds (AREA)
  • Indole Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Данное изобретение относится к новым замещенным тетрациклическим производным тетрагидрофурана, пирролидина и тетрагидротиофена со связывающим сродством к рецепторам серотонина, в частности, рецепторам 5-НТи 5-HT, и по отношению к рецепторам допамина, в частности рецепторам допамина D2, и обладающим свойствами ингибирования повторного поглощения норэпинефрина, фармацевтическим композициям, содержащим соединения в соответствии с данным изобретением, их применению в качестве лекарственного средства, в частности, для профилактики и/или лечения ряда психиатрических и неврологических расстройств, в частности определенных психотических, сердечно-сосудистых и гастрокинетических расстройств, и способам их получения. Соединения в соответствии с данным изобретением могут быть представлены общей формулой (I), а также включают их фармацевтически приемлемые кислотные или основные аддитивные соли, их стереохимически изомерные формы, их N-оксид и их пролекарства, где все заместители таковы, как определены в п.1 формулы изобретения.This invention relates to new substituted tetracyclic derivatives of tetrahydrofuran, pyrrolidine and tetrahydrothiophene with binding affinity for serotonin receptors, in particular 5-HT and 5-HT receptors, and with respect to dopamine receptors, in particular dopamine D2 receptors, and having reuptake inhibitory properties norepinephrine, pharmaceutical compositions containing compounds in accordance with this invention, their use as a medicine, in particular for prevention and / or eniya number of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their preparation. The compounds in accordance with this invention can be represented by the general formula (I), and also include their pharmaceutically acceptable acid or base addition salts, their stereochemically isomeric forms, their N-oxide and their prodrugs, where all substituents are as defined in paragraph. 1 claims.

EA200702626A 2005-05-26 2006-05-24 NEW SUBSTITUTE TETRACYCLIC DERIVATIVES OF TETRAHYDROFURANE, PYRROLIDINE AND TETRAHYDROTHIOPHENE AND THEIR APPLICATION AS A MEDICINE EA200702626A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP05104511 2005-05-26
PCT/EP2006/062612 WO2006125812A1 (en) 2005-05-26 2006-05-24 Novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives and their use as a medicament

Publications (1)

Publication Number Publication Date
EA200702626A1 true EA200702626A1 (en) 2008-04-28

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ID=35004282

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EA200702626A EA200702626A1 (en) 2005-05-26 2006-05-24 NEW SUBSTITUTE TETRACYCLIC DERIVATIVES OF TETRAHYDROFURANE, PYRROLIDINE AND TETRAHYDROTHIOPHENE AND THEIR APPLICATION AS A MEDICINE

Country Status (12)

Country Link
US (1) US20090023721A1 (en)
EP (1) EP1891073A1 (en)
JP (1) JP2008542241A (en)
KR (1) KR20080022084A (en)
CN (1) CN101184759A (en)
AU (1) AU2006251166A1 (en)
BR (1) BRPI0611408A2 (en)
CA (1) CA2604165A1 (en)
EA (1) EA200702626A1 (en)
MX (1) MX2007014857A (en)
NZ (1) NZ562008A (en)
WO (1) WO2006125812A1 (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1701943A1 (en) 2003-12-23 2006-09-20 Myogen, Inc. 5-ht2 receptors modulators, their pharmaceutical compositions and their use for the treatment of cardiovascular and muscle diseases
AU2005313325C1 (en) * 2004-12-07 2011-11-10 Janssen Pharmaceutica N.V. Substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives
AR084867A1 (en) * 2011-02-07 2013-07-10 Lilly Co Eli ACID COMPOUNDS [(5H-PIRROLO [2,1-C] [1,4] BENZODIAZEPIN-11-IL) PIPERAZIN-1-IL] -2,2-DIMETHYLPROPANOIC REPLACED AS 5-HT ANTAGONISTS / INVESTED AGONISTS DUAL
CN111841662B (en) * 2020-06-11 2023-01-20 宁波博汇化工科技股份有限公司 Pre-sulfurization process of hydrorefining catalyst
WO2023023287A1 (en) * 2021-08-18 2023-02-23 The Board Of Regents Of The University Of Texas System Novel heterocyclic compounds as serotonin (5-ht) 5-ht2a and 5-ht2c receptor positive allosteric modulators

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100389298B1 (en) * 1996-04-12 2003-10-30 얀센 파마슈티카 엔.브이. Substituted tetracyclic tetrahydrofuran derivatives
UA52778C2 (en) * 1997-10-10 2003-01-15 Янссен Фармацевтика Н.В. Tetrahydrofurane halogen substituted tetracyclic derivatives, a process for production and compositions on basis thereof
WO2005013969A1 (en) * 2003-07-15 2005-02-17 Janssen Pharmaceutica N.V. Antipsychotic agent with socializing properties
AU2005251948A1 (en) * 2004-06-14 2005-12-22 Janssen Pharmaceutica N.V. Novel tetracyclic tetrahydrofuran derivatives
CA2568752C (en) * 2004-06-23 2013-05-07 Janssen Pharmaceutica N.V. Novel unsaturated tetracyclic tetrahydrofuran derivatives
AU2005313325C1 (en) * 2004-12-07 2011-11-10 Janssen Pharmaceutica N.V. Substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives
WO2006122944A1 (en) * 2005-05-19 2006-11-23 Janssen Pharmaceutica N.V. Selected tetracyclic tetrahydrofuran derivatives containing a cyclic amine side chain

Also Published As

Publication number Publication date
CN101184759A (en) 2008-05-21
WO2006125812A1 (en) 2006-11-30
MX2007014857A (en) 2008-02-14
EP1891073A1 (en) 2008-02-27
AU2006251166A1 (en) 2006-11-30
BRPI0611408A2 (en) 2010-09-08
CA2604165A1 (en) 2006-11-30
US20090023721A1 (en) 2009-01-22
JP2008542241A (en) 2008-11-27
NZ562008A (en) 2010-03-26
KR20080022084A (en) 2008-03-10

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